Ulixertinib (BVD-523)

For research use only.

Catalog No.S7854 Synonyms: VRT752271

27 publications

Ulixertinib (BVD-523) Chemical Structure

CAS No. 869886-67-9

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Size Price Stock Quantity  
USD 147 In stock
USD 447 In stock
USD 997 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Ulixertinib (BVD-523) has been cited by 27 publications

Purity & Quality Control

Choose Selective ERK Inhibitors

Biological Activity

Description Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
ERK1 [1] ERK2 [1]
<0.3 nM
In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A375 cells MXnGeY5kfGmxbjDhd5NigQ>? NY[1UFc{OiCq NHewfHJKdmirYnn0bY9vKG:oIFXST|EwOiCrbjDoeY1idiCDM{e1JINmdGy|IHjhdoJwemmwZzDCMXJCTiCYNkCwSUBufXSjboSgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icHjvd5Bpdy2UU1ugcIV3\WxiYX\0[ZIhOiCqcoOgZpkhS2WubH;tbYN{KEG{cnH5V4NidlSPIG\UTUBqdWGpaX7nJIFv[Wy7c3nzMEBKSzVyPUCuNVQh|ryP M1\QPVI2QTd5OUix
human A375 cells NHn3cnRRem:uaX\ldoF1cW:wIHHzd4F6 MUS3NkBp MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscI9ucWO|IFHydoF6W2OjbmTNJHZVUSCrbXHnbY5oKGGwYXz5d4l{NCCLQ{WwQVAvOThizszN NGLPW2IzPTl5N{m4NS=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-ERK / ERK / RRM2 ; 

PubMed: 28797284     

PANC-1 and BxPC-3 cells were treated with 1 nM of the ERK inhibitor ulixertinib for 24 h. The protein levels of p-ERK, ERK, and RRM2 were detected using western blot analysis.

Growth inhibition assay
Cell viability ; 

PubMed: 30771617     

Caki-1 and 786-O cells were treated with everolimus alone or in combination with ERK inhibitor BVD-523 for 72 h. The cell viability was assessed by CCK-8 assay. **p < 0.01; ***p < 0.001.



Kinase Assay:[1]
- Collapse

ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:

MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
Cell Research:[1]
- Collapse
  • Cell lines: A375 cells
  • Concentrations: ~30 μM
  • Incubation Time: 72 h
  • Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.46 mM)
Ethanol 15 mg/mL (34.61 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.33


CAS No. 869886-67-9
Storage powder
in solvent
Synonyms VRT752271
Smiles CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04488003 Not yet recruiting Drug: Ulixertinib|Drug: Physician''s Choice Advanced Solid Tumor|BRAF Gene Mutation|BRAF Gene Alteration|MEK Mutation|MEK Alteration|MAP2K1 Gene Mutation|MAP2K1 Gene Alteration|MAP2K2 Gene Mutation|MAP2K2 Gene Alteration BioMed Valley Discoveries Inc October 1 2020 Phase 2
NCT04145297 Recruiting Drug: Ulixertinib|Drug: Hydroxychloroquine Gastrointestinal Neoplasms University of Utah|BioMed Valley Discoveries Inc March 17 2020 Phase 1
NCT03698994 Recruiting Other: Pharmacokinetic Study|Drug: Ulixertinib Advanced Malignant Solid Neoplasm|MAPK1 Gene Mutation|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Primary Malignant Central Nervous System Neoplasm|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Primary Malignant Central Nervous System Neoplasm|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor National Cancer Institute (NCI) October 1 2018 Phase 2
NCT02994732 Completed Drug: [14C]-BVD-523 Healthy BioMed Valley Discoveries Inc January 2017 Phase 1
NCT02296242 Completed Drug: BVD-523 Acute Myelogenous Leukemia|Myelodysplastic Syndrome BioMed Valley Discoveries Inc November 2014 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

ERK Signaling Pathway Map

Tags: buy Ulixertinib|Ulixertinib ic50|Ulixertinib price|Ulixertinib cost|Ulixertinib solubility dmso|Ulixertinib purchase|Ulixertinib manufacturer|Ulixertinib research buy|Ulixertinib order|Ulixertinib mouse|Ulixertinib chemical structure|Ulixertinib mw|Ulixertinib molecular weight|Ulixertinib datasheet|Ulixertinib supplier|Ulixertinib in vitro|Ulixertinib cell line|Ulixertinib concentration|Ulixertinib nmr|Ulixertinib in vivo|Ulixertinib clinical trial|Ulixertinib inhibitor|Ulixertinib MAPK inhibitor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID